Journal of Medicinal Chemistry p. 73 - 78 (1991)
Update date:2022-08-11
Topics:
Ricouart, A.
Gesquiere, J. C.
Tartar, A.
Sergheraet, C.
A new class of serine/threonine protein kinase inhibitors was designed by associating, in the same structure, mimics of both the ATP binding site and a protein substrate.Among the several potent antagonists which were obtained, the most active consists of isoquinoline-5-sulfonamide, as ATP mimic, and Ser-Arg6, as peptidic moiety, bound by a -NH(CH2)2NH(CH2)2CO- linker.This compound, with a Ki of 0.1 μM toward protein kinase C (PKC) and 0.004 μM toward cyclic AMP dependent protein kinase (PKA), is respectively 60- and 750-fold more active than the commercial inhibitor H-7.
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(2014)Doi:10.1007/BF00846006
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(2004)Doi:10.1016/S0022-1139(99)00211-0
(2000)Doi:10.1246/bcsj.54.945
(1981)
